KR880701708A - 금속 킬레이트-단백질 공액체를 형성하기 위한 골격이 다중치환된 킬레이트 - Google Patents
금속 킬레이트-단백질 공액체를 형성하기 위한 골격이 다중치환된 킬레이트Info
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- KR880701708A KR880701708A KR1019880700490A KR880700490A KR880701708A KR 880701708 A KR880701708 A KR 880701708A KR 1019880700490 A KR1019880700490 A KR 1019880700490A KR 880700490 A KR880700490 A KR 880700490A KR 880701708 A KR880701708 A KR 880701708A
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- diethylenetriamine
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- C07C331/22—Isothiocyanates having isothiocyanate groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
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- A61K51/04—Organic compounds
- A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
- A61K51/0478—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group complexes from non-cyclic ligands, e.g. EDTA, MAG3
- A61K51/048—DTPA (diethylenetriamine tetraacetic acid)
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- A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
- A61K51/1093—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies
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- C07C211/02—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
- C07C211/15—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
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- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
- C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
- C07C229/16—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
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- C07C233/00—Carboxylic acid amides
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- C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
- C07C233/42—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
- C07C233/43—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2121/00—Preparations for use in therapy
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2123/00—Preparations for testing in vivo
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
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Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 R1이 파라-니트로벤질이고, R3,4가 본 명세서에 기재된 것과 아릴/일킬기인 다중치환된 딩텔렌트리아민 제조를 위한 반응식을 나타낸 것이다. R3,4가 메틸기인 경우, 반응식중의 디에틸렌트리아민 생성물은 표1의 화합물(d)이다.
제2도는 PG가 보호기(하기 참조)를 나타내고, R 및 R'가 파라-니트로벤질 또는 각각 본 명세서에 기재된 것과 같은 아릴/알킬기인 다중치환된 디에틸렌트리아민 제조를 위한 반응식을 나타낸 것이다. R이 파라-니트로벤질이고, R'가 메틸인 경우, 생성물 디에틸렌트리아민은 표1의 화합물(a)이다. R이 메틸이고, R'가 파라-니트로벤질인 경우, 생성물 디에틸렌트리아민 표1의 화합물(C)이다.
Claims (14)
- (a)아미노 보호 알파 아미노산을 아미노산 아미드와 반응시키는 단계, (b)보호된 아미노산을 탈보호시키는 단계, (c)단계(b)에서 얻은 생성물을 환원시켜 다중치환된 디에틸렌트리아민을 제조하는 단계및 (d)상기 디에틸렌트리아민을 할로아세트산 또는 할로아세테이트 에스테르로 알킬화함으로써 목적하는 다중치환된 디에틸렌트리아민펜타아세트산 또는 그의 에스테르로 전환시키는 일련의 단계로 되는 다중치환된 디에틸렌트리아민펜타아세트산 킬레이트의 제조방법
- (a)아미노 보호 알파 아미노산을 알파 아미노케톤과 반응시키는 단계, (b)생성된 케톤을 메톡실아민과 반응시킴으로써 옥심 에테르로 전환시키는 단계 및 (c)생성된 옥심 에테르를 탈보호하고, 이어서 탈보호된 옥심 에테르를 환원시켜서 할로아세트산 또는 에스테르로 알킬화한 후 목적하는 다중치환된 디에틸렌트리아민펜타아세트산 또는 그의 에스테르를 얻는 디에틸렌트리아민을 제조하는 단계로 되는 다중치환된 디에틸렌트리아민펜타아세트산 킬레이트의 제조방법
- 디에틸렌트리아민펜타아세트산(DTPA)의 탄소 골격에 결합되는 1개의 측쇄를 갖고, 약 1-7 pH범위를 갖는 수용액 중에서 안정하고 단백질의 아미노산 잔기와 직접 반응하여 pH 약 6-11의 공액 pH에서 안정한 공유 결합을 형성하는 기능기를 함유하고, DTPA의 탄소 골격에 결합된 1-8의 탄소 원자수를 갖는 1개 이상의 부가적인 측쇄를 갖는 하기 일반식(2) 또는 (3)으로 표시되는 다중치환된 DTPA
- 제3항에 있어서, 기능기가 할로아세트아미드인 다중치환된 DTPA
- 제3항에 있어서, 기능기가 이소티오시아네이트인 다중치환된 DTPA
- 제3항에 있어서, 기능기가 N-히드록시숙신아미드 에스테르인 다중치환된 DTPA
- 제3항에 있어서, R1-R4, R1'-R4'기들이 다음가 같은 다중치환된 DTPA여기서, SCNBz는 파라-이소티오시아네이트벤질기이다.
- 단백질과 공액된 제3항에 의한 DTPA
- 제8항에 있어서, 상기 단백질의 모노-또는 폴리-클로날 항체 또는 이들의 단편인 DTPA
- 방사성 원소로 표지화된 제9항에 의한 DTPA
- 제10항에 있어서, 방사성 표지가 In-111, Y-90, Bi-212, Ga-68 및 Sc-47로 되는 군중에서 선택되는 DTPA
- 숙주중의 표적 부위에서 방사선 치료 효과 또는 라디오이미징(radioimaging)효과를 얻는데 유효한양의 제11항의 화합물을 숙주에 투여하는 것으로 되는 숙주중의 표적 부위에 방사성 원소 표지화 화합물을 도출시키는 방법
- 트리아민의 탄소 골격에 결합된 적어도 2개의 측쇄를 갖고, 니트로기를 함유하는 하기 일반식의 다중치환된 디에틸렌트리아민
- 제13항에 있어서, R1-R4, R1'-R4'가 다음과 같은 다중치환된 디에틸렌트리아민여기서, SCNBz는 파라-이소티오시아네이트벤질기이다.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US06/903,723 US4831175A (en) | 1986-09-05 | 1986-09-05 | Backbone polysubstituted chelates for forming a metal chelate-protein conjugate |
US903723 | 1986-09-05 | ||
PCT/US1987/002207 WO1988001618A1 (en) | 1986-09-05 | 1987-09-04 | Backbone polysubstituted chelates for forming a metal chelate-protein conjugate |
CA000594072A CA1338721C (en) | 1986-09-05 | 1989-03-17 | Backbone polysubstituted chelates for forming a metal chelate-protein conjugate |
Publications (2)
Publication Number | Publication Date |
---|---|
KR880701708A true KR880701708A (ko) | 1988-11-04 |
KR920003590B1 KR920003590B1 (ko) | 1992-05-04 |
Family
ID=25672531
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1019880700490A KR920003590B1 (ko) | 1986-09-05 | 1987-09-04 | 금속 킬레이트-단백질 결합체를 형성하기 위한 다중치환된 골격을 갖는 킬레이트 |
Country Status (9)
Country | Link |
---|---|
US (1) | US4831175A (ko) |
EP (1) | EP0328529B1 (ko) |
JP (2) | JP2555391B2 (ko) |
KR (1) | KR920003590B1 (ko) |
AT (2) | ATE144496T1 (ko) |
AU (1) | AU611105B2 (ko) |
CA (1) | CA1338721C (ko) |
DE (3) | DE3788961T2 (ko) |
WO (1) | WO1988001618A1 (ko) |
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US4622420A (en) * | 1980-03-18 | 1986-11-11 | The Regents Of The University Of California | Chelating agents and method |
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US4472509A (en) * | 1982-06-07 | 1984-09-18 | Gansow Otto A | Metal chelate conjugated monoclonal antibodies |
SE8301395L (sv) * | 1983-03-15 | 1984-09-16 | Wallac Oy | Kelatiserande foreningar med funktionella grupper vilka tillater kovalent koppling till bio-organiska molekyler |
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1986
- 1986-09-05 US US06/903,723 patent/US4831175A/en not_active Expired - Lifetime
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1987
- 1987-09-04 AT AT92114713T patent/ATE144496T1/de active
- 1987-09-04 WO PCT/US1987/002207 patent/WO1988001618A1/en active IP Right Grant
- 1987-09-04 DE DE3788961T patent/DE3788961T2/de not_active Expired - Lifetime
- 1987-09-04 DE DE3751788T patent/DE3751788T2/de not_active Expired - Lifetime
- 1987-09-04 DE DE3751936T patent/DE3751936T2/de not_active Expired - Lifetime
- 1987-09-04 AT AT91122418T patent/ATE137214T1/de not_active IP Right Cessation
- 1987-09-04 AU AU80743/87A patent/AU611105B2/en not_active Ceased
- 1987-09-04 JP JP62505982A patent/JP2555391B2/ja not_active Expired - Lifetime
- 1987-09-04 KR KR1019880700490A patent/KR920003590B1/ko not_active IP Right Cessation
- 1987-09-04 EP EP87906504A patent/EP0328529B1/en not_active Expired - Lifetime
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1989
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JP2555391B2 (ja) | 1996-11-20 |
EP0328529A1 (en) | 1989-08-23 |
EP0328529B1 (en) | 1994-01-26 |
JPH08231474A (ja) | 1996-09-10 |
DE3751788T2 (de) | 1996-11-28 |
DE3751936T2 (de) | 1997-04-03 |
WO1988001618A1 (en) | 1988-03-10 |
AU611105B2 (en) | 1991-06-06 |
DE3751788D1 (de) | 1996-05-30 |
JP2659351B2 (ja) | 1997-09-30 |
DE3751936D1 (de) | 1996-11-28 |
US4831175A (en) | 1989-05-16 |
DE3788961D1 (de) | 1994-03-10 |
ATE144496T1 (de) | 1996-11-15 |
EP0328529A4 (en) | 1991-03-20 |
DE3788961T2 (de) | 1994-07-14 |
CA1338721C (en) | 1996-11-12 |
AU8074387A (en) | 1988-03-24 |
ATE137214T1 (de) | 1996-05-15 |
JPH02501385A (ja) | 1990-05-17 |
KR920003590B1 (ko) | 1992-05-04 |
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